KB-141 [Ligand Id: 2638] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL41036
  • Thyroid hormone receptor-α/Thyroid hormone receptor alpha in Human [ChEMBL: CHEMBL1860] [GtoPdb: 588] [UniProtKB: P10827]
  • 8.14
1 CHEMBL41036_lig_chart_1 Thyroid hormone receptor alpha Human
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  • Thyroid hormone receptor-β/Thyroid hormone receptor beta-1 in Human [ChEMBL: CHEMBL1947] [GtoPdb: 589] [UniProtKB: P10828]
  • 9.43
2 CHEMBL41036_lig_chart_2 Thyroid hormone receptor beta-1 Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Thyroid hormone receptor-α/Thyroid hormone receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1860] [GtoPdb: 588] [UniProtKB: P10827]
ChEMBL Displacement of [125I]3,5,3'-triiodo-L-thyronine from His-tagged human recombinant TRalpha1 by scintillation proximity assay B 8.11 pKi 7.79 nM Ki J. Med. Chem. (2008) 51: 7075-7093 [PMID:18975928]
ChEMBL Displacement of [125I]T3 from recombinant thyroid hormone receptor alpha expressed in sf9 cells by scintillation proximity assay B 8.14 pKi 7.18 nM Ki Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 15490-15495 [PMID:17878314]
ChEMBL Binding affinity to TRalpha1 B 8.14 pKi 7.18 nM Ki J. Med. Chem. (2012) 55: 5649-5675 [PMID:22512468]
ChEMBL Inhibition of thyroid hormone receptor alpha B 7.6 pIC50 25.12 nM IC50 Bioorg. Med. Chem. (2007) 15: 4609-4617 [PMID:17467994]
GtoPdb - - 7.6 pIC50 - - - J Med Chem (2003) 46: 1580-8 [PMID:12699376]
ChEMBL Concentration required to inhibit 50% of I-T3 binding to hTR1 (Thyroid hormone receptor alpha) was determined B 7.6 pIC50 25 nM IC50 J. Med. Chem. (2003) 46: 1580-1588 [PMID:12699376]
ChEMBL Inhibitory concentration against cloned human thyroid hormone receptor alpha 1 B 7.6 pIC50 25 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 4579-4584 [PMID:16099653]
ChEMBL Binding affinity at human thyroid hormone receptor alpha 1 expressed in CHOK1 cells B 7.6 pIC50 25 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 4131-4134 [PMID:17543524]
ChEMBL Effect on CHO-K1 cells stably transfected with Thyroid hormone receptor alpha (TRalpha1) and an alkaline phosphate reporter gene downstream thyroid response element TRAF-alpha1 was determined B 7.96 pEC50 11 nM EC50 J. Med. Chem. (2003) 46: 1580-1588 [PMID:12699376]
ChEMBL Agonist activity at recombinant His6-tagged THR-alpha (unknown origin) expressed in Escherichia coli BL21(DE3) co-expressing RXR preincubated for 30 mins assessed as biotin-GRIP1 peptide recruitment by HTRF assay B 8.3 pEC50 5 nM EC50 J. Med. Chem. (2014) 57: 3912-3923 [PMID:24712661]
ChEMBL Agonist activity at human thyroid hormone receptor alpha expressed in CV1 cells by TRE-luciferase assay F 8.35 pEC50 4.5 nM EC50 Bioorg. Med. Chem. Lett. (2008) 18: 3919-3924 [PMID:18585912]
Thyroid hormone receptor-β/Thyroid hormone receptor beta-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1947] [GtoPdb: 589] [UniProtKB: P10828]
ChEMBL Displacement of [125I]T3 from recombinant thyroid hormone receptor beta expressed in sf9 cells by scintillation proximity assay B 9.43 pKi 0.37 nM Ki Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 15490-15495 [PMID:17878314]
ChEMBL Binding affinity to TRbeta1 B 9.43 pKi 0.37 nM Ki J. Med. Chem. (2012) 55: 5649-5675 [PMID:22512468]
ChEMBL Displacement of [125I]3,5,3'-triiodo-L-thyronine His-tagged human recombinant TRbeta1 by scintillation proximity assay B 9.62 pKi 0.24 nM Ki J. Med. Chem. (2008) 51: 7075-7093 [PMID:18975928]
ChEMBL Concentration required to inhibit 50% of I-T3 binding to hTR1 (Thyroid hormone receptor beta) was determined B 8.96 pIC50 1.1 nM IC50 J. Med. Chem. (2003) 46: 1580-1588 [PMID:12699376]
ChEMBL Inhibitory concentration against cloned human thyroid hormone receptor beta 1 B 8.96 pIC50 1.1 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 4579-4584 [PMID:16099653]
ChEMBL Binding affinity at human thyroid hormone receptor beta-1 expressed in CHOK1 cells B 8.96 pIC50 1.1 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 4131-4134 [PMID:17543524]
GtoPdb - - 8.96 pIC50 - - - Proc Natl Acad Sci USA (2003) 100: 10067-72 [PMID:12888625]
ChEMBL Inhibition of human thyroid hormone receptor beta 1 B 8.96 pIC50 1.1 nM IC50 Bioorg. Med. Chem. (2007) 15: 5251-5261 [PMID:17524652]
ChEMBL Inhibition of thyroid hormone receptor beta B 8.96 pIC50 1.1 nM IC50 Bioorg. Med. Chem. (2007) 15: 4609-4617 [PMID:17467994]
ChEMBL Agonist activity at recombinant His6-tagged THR-beta (unknown origin) expressed in Escherichia coli BL21(DE3) co-expressing RXR preincubated for 30 mins assessed as biotin-GRIP1 peptide recruitment by HTRF assay B 7.64 pEC50 23 nM EC50 J. Med. Chem. (2014) 57: 3912-3923 [PMID:24712661]
ChEMBL Effect on CHO-K1 cells stably transfected with Thyroid hormone receptor beta and an alkaline phosphate reporter gene downstream thyroid response element TRAF-beta1 was determined B 8.46 pEC50 3.5 nM EC50 J. Med. Chem. (2003) 46: 1580-1588 [PMID:12699376]
ChEMBL Agonist activity at human thyroid hormone receptor beta expressed in CV1 cells by TRE-luciferase assay F 8.95 pEC50 1.12 nM EC50 Bioorg. Med. Chem. Lett. (2008) 18: 3919-3924 [PMID:18585912]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]